Method for preparing acetyl captopril

Abstract

The invention relates to the technical field of medicines, and provides a method for preparing acetyl captopril. The method has the advantages that the method includes technologies for carrying out addition on thioacetic acid and methacrylic acid, then carrying out separation on the thioacetic acid and the methacrylic acid and preparing a captopril intermediate 'D-ethanethioate-2-methyl propionylchloride' from the thioacetic acid, the methacrylic acid and thionyl chloride by means of acylating chlorination, as proved by repeated tests, acetone which is an organic solvent is replaced with waterwhich is an inorganic solvent, accordingly, the safety of preparation technologies can be improved, and environmental pollution can be reduced; resolving agents are screened by the aid of half-amount(or full-amount) resolving processes, accordingly, the screening efficiency can be improved, and the screening frequencies can be reduced; recycling systems are improved, accordingly, the material input can be reduced, the utilization rate of precious raw materials can be increased, and emission of pollutants can be obviously reduced; technological conditions of temperatures, pressures, reactiontime and the like in technologic control procedures are determined, and accordingly the quality stability of industrial production can be guaranteed.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method of acetylcaptopril. Background technique [0002] Captopril (I, captopril) is the first clinical application of angiotensin-converting enzyme (ACE) inhibitors, mainly used for the treatment of hypertension, heart failure and other diseases. The product captopril intermediate of the present invention "3-acetylthio-2-methylpropionyl chloride" referred to as "acetylcaptopril" is a key intermediate for the preparation of captopril raw materials, mainly used for the preparation of captopril Puli API. [0003] At present, the preparation of captopril intermediates at home and abroad generally uses organic solvent acetone as a solvent. Acetone is a flammable substance with high risk and easy to cause environmental pollution. Acetone belongs to Class 3.1 low-flash point flammable liquid in the classification of hazardous chemicals. It is extremely volatile and can cause exp...

AI Technical Summary

Problems solved by technology

Use non-toxic, non-polluting, safe to use, and extensive resources of inorganic solvent-water to replace the organic solvent-acetone in the traditional production process of acetylcaptopril, to solve the problems of high risk and large environmental pollution in the traditional preparation process, production 30% cost reduction, safe and reliable, energy saving and environmental protection

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